具有SAH水解酶抑制活性的去甲瑞斯托霉素类似物的合成用于抗疟药物的开发。

Synthesis of noraristeromycin analogues possessing SAH hydrolase inhibitory activity for the development of antimalaria agents.

作者信息

Kojima Hiroharu, Yamaguchi Tsuyoshi, Kozaki Atsushi, Nakanishi Masayuki, Ueno Yoshihito, Kitade Yukio

机构信息

Laboratory of Molecular Biochemistry, Department of Biomolecular Science, Faculty of Engineering, Gifu University, Yanagido 1-1, Gifu 501-1193, Japan.

出版信息

Nucleic Acids Res Suppl. 2002(2):141-2. doi: 10.1093/nass/2.1.141.

DOI:10.1093/nass/2.1.141

PMID:12903145

Abstract

Noraristeromycin analogues such as 3',4'-anhydronoraristeromycins, 2-amino-3',4'-anhydronoraristeromycin and N6-cyclopropylnoraristeromycin were synthesized and their inhibitory activity against human and Plasmodium falciparum (P. falciparum) recombinant SAH hydrolase was investigated. Among them, 3',4'-anhydronoraristeromycin showed inhibitory activity against human recombinant S-adenosyl-L-homocysteine hydrolase (Ki = 12.4 microM, Kinact = 0.55 min-1).

摘要

合成了诺里霉素类似物，如3',4'-脱水诺里霉素、2-氨基-3',4'-脱水诺里霉素和N6-环丙基诺里霉素，并研究了它们对人和恶性疟原虫重组S-腺苷-L-高半胱氨酸水解酶的抑制活性。其中，3',4'-脱水诺里霉素对人重组S-腺苷-L-高半胱氨酸水解酶表现出抑制活性（Ki = 12.4 microM，Kinact = 0.55 min-1）。